JP2006298831A - COATED alpha-LIPOIC ACID POWDER AND METHOD FOR PRODUCING THE SAME, AND FOOD COMPRISING alpha-LIPOIC ACID - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a method effectively producing high quality α-lipoic acid powder excellent in stability with passage of the time after production and to provide a method for producing the coated α-lipoic acid powder with suppressed deterioration of the active ingredients and excellent in stability with passage of the time and to provide a food containing α-lipoic acid. <P>SOLUTION: The coated α-lipoic acid powder has 1-10 μm of uniform coated layer of fat composed of a fat based material on the surface of the α-lipoic acid powder particles and has 50-300 μm of average particle diameter. The method for producing the coated α-lipoic acid powder comprises a process mixing and agitating the α-lipoic acid powder with the fat having excess 40°C of melting point and 0.1-50 μm of average particle diameter under conditions under which collision average load attains 0.01 to 10 N. The food comprising the α-lipoic acid comprises the coated α-lipoic acid powder. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to an α-lipoic acid powder coating useful as a health food material and the like, a method for producing the same, and an α-lipoic acid-containing food.

Alpha lipoic acid is present in the mitochondria of the cells that make up the body, and is an essential nutrient for cell respiration and energy production. Currently, alpha lipoic acid is used in health foods such as pharmaceuticals, cosmetics and supplements. For example, Patent Document 1 includes lipoic acid and carnitine, and in order to reverse the signs of aging by restoring mitochondrial function of aging cells without concomitantly increasing the metabolic production of reactive oxygen species. Orally administrable compositions are disclosed.
Special table 2001-508804 gazette

  Alpha lipoic acid is also called thioctic acid. α-Lipoic acid is mainly produced by a synthetic method and is usually supplied in the form of crystal powder. Such crystal powder is weak to heat and has a property of being easily polymerized and deteriorated when exposed to ultraviolet rays and oxygen. Furthermore, since it has a large specific surface area, it has poor fluidity and is compressed into tablets or filled into capsules. Have the problem of poor processability when working. On the other hand, Patent Document 1 discloses an example of use in combination with a pharmaceutically acceptable excipient such as gelatin or oil. It is hard to say that it has been solved.

  As a result of intensive studies to solve the problems existing in the prior art, the present inventors have obtained a powder having a specific melting point and particle diameter and having a specific range of collision average load. Thus, the α-lipoic acid powder coating was successfully produced by mixing and stirring with the α-lipoic acid powder. Further, in the α-lipoic acid powder coating produced by this method, a uniform and thin oil-based coating layer is formed on the surface of the powder particles of α-lipoic acid, and the α-lipoic acid coating layer is formed by the oil-based coating layer. It was found that the deterioration was suppressed and the stability over time was excellent. And based on these knowledge, it came to complete this invention.

  An object of the present invention is to provide a method for producing an α-lipoic acid powder coating that can efficiently produce a high-quality α-lipoic acid powder coating that is excellent in stability over time after production. It is in. Another object is to provide an α-lipoic acid powder coating and an α-lipoic acid-containing food that suppresses the deterioration of active ingredients and is excellent in stability over time.

  In order to achieve the above object, the method for producing an α-lipoic acid powder coating according to claim 1 is characterized in that an α-lipoic acid powder coating having an oil-based coating layer on the surface of powder particles of α-lipoic acid. This is a production method, in which a powder of an oil-based coating material having a melting point of 40 ° C. or higher and an average particle diameter of 0.1 to 50 μm is subjected to alpha lipolysis with a collision average load of 0.01 to 10 N. The gist is to mix and stir with the acid powder.

  According to this method, it is possible to form a uniform and thin oil-based coating layer on the surface of α-lipoic acid powder particles very simply and inexpensively. The oil-based coating layer has an action of blocking α-lipoic acid present inside the α-lipoic acid powder coating from the outside of the coating. By this action, α-lipoic acid as an active ingredient is effectively protected from moisture absorption, oxygen, and deterioration due to light, so that the stability over time of the active ingredient is enhanced.

  The α-lipoic acid powder coating according to claim 2 is an α-lipoic acid powder coating manufactured by the method according to claim 1, wherein the coating is a powder particle of the α-lipoic acid. The gist of the present invention is that it has a homogeneous oil-based coating layer having a thickness of 1 to 10 μm made of the oil-based coating material on the surface thereof and an average particle diameter in the range of 50 to 300 μm.

  The gist of the α-lipoic acid-containing food according to claim 3 contains the α-lipoic acid powder coating according to claim 2.

  ADVANTAGE OF THE INVENTION According to this invention, the manufacturing method of the alpha lipoic acid powder coating material which can manufacture efficiently the high quality alpha lipoic acid powder coating material excellent in the temporal stability after manufacture can be provided. Moreover, according to this invention, degradation of an active ingredient is suppressed and the alpha lipoic acid powder coating material and alpha lipoic acid containing foodstuffs which were excellent in stability with time can be provided.

Hereinafter, the alpha lipoic acid powder coating material of this invention, its manufacturing method, and one Embodiment which actualized the alpha lipoic acid containing foodstuff are described.
The α-lipoic acid powder coating according to this embodiment has an oil-based coating layer on the surface of α-lipoic acid powder particles. For this reason, in this α-lipoic acid powder coating, α-lipoic acid as an active ingredient is physically blocked from ultraviolet rays, moisture and oxygen in the air via the oil-based coating layer. It can be a health food material or α-lipoic acid-containing food that is suppressed in deterioration of acid and has excellent stability over time.

  The α-lipoic acid powder is not particularly limited as long as it is a dry powder product, and may be dried by any method such as a vacuum drying method, a spray drying method, or a freeze drying method. As the α-lipoic acid powder, a powder having a particle diameter of 10 to 350 μm and an average particle diameter of about 40 to 280 μm is preferably used.

  As the oil-based coating material for forming the oil-based coating layer, a material having a melting point of 40 ° C. or higher is used. An oil-based coating material having a melting point of less than 40 ° C. may lead to an undesirable situation such as the particles of the α-lipoic acid powder coating being fused together in a high temperature environment such as summer. Examples of the oil-based coating materials include animal oils such as beef tallow, pork tallow and fish oil, vegetable oils such as soybean oil, rapeseed oil, cottonseed oil, corn oil and coconut oil, hydrogenated oils of these animal and vegetable oils, rice wax, beeswax, carnauba wax, Waxes such as canderia, fatty acid metal salts, fatty acids, phospholipids, glycolipids, monoglycerides, diglycerides and the like can be used, but it is particularly preferable to use vegetable hardened fats and oils. These oil-based coating materials may be used alone or in combination of two or more. The oil-based coating material powder needs to have an average particle diameter of 0.1 to 50 μm. When an oil-based coating material having an average particle diameter outside the above range is used, it becomes difficult to form a homogeneous oil-based coating layer having a desired thickness.

  The manufacturing method of the alpha lipoic acid powder coating material of this embodiment includes the process of mixing and stirring the alpha lipoic acid powder and the oil-based coating material powder. In this step, an oil-based coating layer is formed on the surface of the α-lipoic acid powder particles. This step is performed using, for example, a stirrer 10 shown in FIG. The stirrer 10 includes a main shaft stirring blade 11 and a sub-shaft stirring blade 12 that stirs in a direction orthogonal to the main shaft stirring blade 11 in the stirring tank 13. The lipoic acid powder and the oil-based coating material powder are charged, and the α-lipoic acid powder and the oil-based coating material powder are mixed and stirred in the stirring tank 13 while colliding with each other. At this time, powder particles of the oil-based coating material are coated on the surface of the α-lipoic acid powder particles, and an oil-based coating layer is formed on the surface of each α-lipoic acid powder coating.

  In this step, the α lipoic acid powder and the oil-based coating material powder need to be mixed and stirred under conditions such that the collision average load is 0.01 to 10 N (Newton). If the collision average load at the time of mixing and stirring deviates from the above range, it becomes difficult to form a uniform oil-based coating layer having a desired thickness. The collision average load is obtained by the following formula 1.

ただし、上記式中、Ｆは衝突平均荷重（Ｎ）、ｒ_１及びｒ_２はαリポ酸及び油脂系被覆材料の各粒子の平均半径（ｍ）、ｍ_１及びｍ_２はαリポ酸及び油脂系被覆材料の各粒子の平均質量（ｋｇ）、Ｙ_１及びＹ_２はαリポ酸及び油脂系被覆材料の各粒子のヤング率（ｋｇ／ｍ・sec^２）、ν_１及びν_２はαリポ酸及び油脂系被覆材料の各粒子のポアソン比、Ｖは衝突速度（ｍ／sec）を示す。

However, in the above formula, F is the collision Average Load (N), r ₁ and r ₂ are the average radius of each particle of the α-lipoic acid and oil-based coating material (m), m ₁ and m ₂ are α-lipoic acid and oils The average mass (kg) of each particle of the system coating material, Y ₁ and Y ₂ are α-lipoic acid and Young's modulus (kg / m · sec ² ) of each particle of the oil-based coating material, and ν ₁ and ν ₂ are α lipo Poisson's ratio of each particle of acid and oil-based coating material, V indicates a collision speed (m / sec).

  The adjustment of the collision average load differs depending on the types of the stirring blades 11 and 12, but for example, the peripheral speed of the main shaft stirring blade 11 is about 0.1 to 20 m / second, and the peripheral speed of the auxiliary shaft stirring blade 12 is 0.01 to 10 m. / Second can be adjusted. The mixing ratio of the α lipoic acid powder and the oil-based coating material powder is usually selected in the range of 40:60 to 99.0: 1.0 by weight. The preferable mixing ratio varies depending on the average particle diameter of the α-lipoic acid powder coating. That is, when the average particle diameter of the α lipoic acid powder coating is R μm, the amount of the oil-based coating material added to the total weight of the α lipoic acid powder coating is 300 / R to 3000 / R wt%. Is preferred. The mixing and stirring time varies depending on the stirring conditions and cannot be determined in general, but usually about 30 to 60 minutes is sufficient.

  In the production method of the present embodiment, in order to suppress the degradation of α-lipoic acid during production, a cooling gas containing 20 ° C. or less containing as little oxygen as possible, for example, in a cooled nitrogen gas atmosphere or a cooled carbon dioxide atmosphere It is preferable to carry out mixing and stirring. As a result, the temperature of α-lipoic acid can be suppressed to 30 ° C. or lower throughout the mixing and stirring step, and deterioration of α-lipoic acid due to temperature rise and moisture absorption during mixing and stirring can be suppressed. In this way, an α-lipoic acid powder coating having an average particle diameter of 50 to 300 μm having a homogeneous oil-based coating layer having a thickness of 1 to 10 μm on the surface of the α-lipoic acid powder particles is efficiently produced. In the α-lipoic acid powder coating of this embodiment, the content of the oil-based coating material is 300 / R to 3000 / R wt% when the average particle diameter of the α-lipoic acid powder coating is R μm. It is preferable that it exists in the range.

  The α-lipoic acid-containing food of this embodiment contains the α-lipoic acid powder coating. α-Lipoic acid-containing foods include not only health foods with dosage forms such as hard capsules, soft capsules, powder preparations, tableting preparations, but also beverages dissolved in water and hot water, as well as general health foods as well as health foods. It can also be added to processed foods.

The effects exhibited by the embodiment will be described below.
According to the production method of the present embodiment, it is possible to form a uniform and thin oil-based coating layer on the surface of the α-lipoic acid powder particles very simply and inexpensively. For this reason, in the resulting α-lipoic acid powder coating, the α-lipoic acid present inside the coating and the outside of the coating are blocked by the oil-based coating layer. It is possible to protect α-lipoic acid from deterioration due to. Therefore, it is possible to easily produce an α-lipoic acid powder coating capable of easily increasing the stability of active ingredients over time.

  -Since the manufacturing method of this embodiment does not include a step of pulverizing powder, α-lipoic acid is not exposed on the surface of the α-lipoic acid powder coating, and a product having a uniform particle size is obtained. Easy to manufacture. Moreover, when manufacturing by mixing stirring using the stirrer 10, since the process of heating (alpha) lipoic acid to high temperature (for example, 60 degreeC or more) is not essential, it is possible to suppress easily deterioration of (alpha) lipoic acid. . Furthermore, since it is easy to form the thickness of the oil-based coating layer uniformly, a high-quality α-lipoic acid powder coating can be easily produced. On the other hand, when forming an oil-based coating layer, the drying step can be omitted compared to the case of a water-soluble coating layer, so there is no need to expose α-lipoic acid to a high temperature and high humidity state for a long time. In particular, it is possible to increase the stability of α-lipoic acid.

  -According to the manufacturing method of this embodiment, since it is easy to form an oil-based coating layer thinly, an α-lipoic acid powder coating containing α-lipoic acid at a high content of 40 to 99% by weight is provided. It is possible to manufacture. In particular, an α-lipoic acid powder coating containing 60% by weight or more of α-lipoic acid is very excellent in terms of cost and usability.

  The α-lipoic acid powder coating of this embodiment may be dissolved in, for example, water or hot water and may be drunk as a beverage, or may be ingested as a powder. It can also be used for general processed foods. In particular, since the stability over time is high, it is important to be able to expand into the general food field. In addition, in the field of health foods having product forms such as hard capsules, soft capsules, and tableting preparations, the product quality assurance period can be greatly extended. Moreover, the filling property to a hard capsule and tableting property are also favorable.

EXAMPLES Next, although an Example demonstrates this invention still in detail, this invention is not limited at all by these examples.
Example 1
80 parts by weight of α-lipoic acid powder having an average particle diameter of 100 μm and 20 parts by weight of powdered rapeseed oil (melting point 65 ° C.) having an average particle diameter of 10 μm were mixed and stirred using the stirrer 10 shown in FIG. The mixing and stirring conditions are as follows: the diameter D1 of the main shaft stirring blade 11 is 1.1 m, the diameter D2 of the sub shaft stirring blade 12 is 0.3 m, the peripheral speed of the main shaft stirring blade 11 is 5 m / sec, The speed was set to 1 m / second, and the nitrogen gas cooled to 10 ° C. was blown into the stirring tank 13 of the stirrer 10 while adjusting the average collision load to 0.06 N. The average collision load was calculated on the assumption that the α lipoic acid powder particles collided with the wall surface.

  By stirring and mixing for about 40 minutes, an α-lipoic acid powder coating with an average particle size of 120 μm was obtained. Next, when the cross section of the particle | grains of the obtained (alpha) lipoic acid powder coating material was image | photographed with the electron microscope, it had the thickness of the oil-based coating layer of an average of 5 micrometers. Further, the obtained α-lipoic acid powder coating had high fluidity and good handleability as compared with the α-lipoic acid powder used as a raw material.

(Example 2)
An α-lipoic acid powder coating having an average particle size of 110 μm was produced in the same manner as in Example 1 except that the amounts of α-lipoic acid powder and rapeseed hydrogenated oil powder were changed to 60 parts by weight and 40 parts by weight, respectively. Things were obtained. The obtained α-lipoic acid powder coating had an average thickness of the oil-based coating layer of 8 μm, high fluidity, and good handleability.

(Example 3)
The α lipoic acid powder coating obtained in Example 1 was encapsulated in a hard capsule made of gelatin to obtain a hard encapsulated product.

Example 4
The α lipoic acid powder coating obtained in Example 2 was encapsulated in a hard capsule made of gelatin to obtain a hard encapsulated product.

(Comparative Example 1)
A coating was produced in the same manner as in Example 1 except that the average collision load was changed to 0.005N. Next, when the obtained coating was observed with an electron microscope, almost no oil-based coating layer was formed.

(Comparative Example 2)
Except for changing the average collision load to 12N, an attempt was made to produce a coating in the same manner as in Example 1. As a result, most of the powder used as a raw material adhered to the wall surface of the stirring tank 13, and a good coating was obtained. Couldn't get.

(Comparative Example 3)
Add 85 parts by weight of α-lipoic acid powder to 15 parts by weight of rapeseed hydrogenated oil heated to 80 ° C., and after cooling and solidification, grind with a mixer until all particles have a diameter of 300 μm or less. Thus, a coating was obtained.

(Comparative Example 4)
The alpha lipoic acid powder used in Example 1 was referred to as Comparative Example 4.
(Comparative Example 5)
The α lipoic acid powder of Comparative Example 4 was encapsulated in a hard capsule made of gelatin to obtain a hard encapsulated product. Note that the α lipoic acid powder used in this example had poor fluidity, and therefore poor workability during the enclosing operation.

<Evaluation of stability over time>
The coatings obtained in Examples 1 and 2 and Comparative Examples 1, 3 and 4 and the hard encapsulated products obtained in Examples 3 and 4 and Comparative Example 5 were each in air at a temperature of 40 ° C. and a humidity of 75%. And stored open for the period shown in Tables 1 and 2. The residual ratio of α-lipoic acid in each coating and hard-encapsulated product after storage for a predetermined period was quantified by liquid chromatography. The results are shown in Tables 1 and 2, respectively.

さらに、前記実施形態より把握できる技術的思想について以下に記載する。

Further, the technical idea that can be grasped from the embodiment will be described below.

The method for producing an α-lipoic acid powder coating according to claim 1, wherein the powder of the oil-based coating material and the α-lipoic acid powder are mixed and stirred in a cooling gas atmosphere of 20 ° C. or less. .
The content of the oil-based coating material is 300 / R to 3000 / R wt% [wherein R represents an average particle diameter (μm) of the α lipoic acid powder coating]. Alpha lipoic acid powder coating.

Sectional drawing which shows typically the stirrer used by embodiment and the Example.

Claims (3)

A method for producing an α-lipoic acid powder coating having an oil-based coating layer on the surface of α-lipoic acid powder particles,
In this method, a powder of an oil-based coating material having a melting point of 40 ° C. or higher and an average particle size of 0.1 to 50 μm is mixed and stirred with α lipoic acid powder at an impact average load of 0.01 to 10 N. A process for producing an α-lipoic acid powder coating. An α-lipoic acid powder coating produced by the method according to claim 1,
The coating has a homogeneous oil-based coating layer having a thickness of 1 to 10 μm made of the oil-based coating material on the surface of the α-lipoic acid powder particles, and has an average particle diameter in the range of 50 to 300 μm. An alpha lipoic acid powder coating characterized by the above.   An α-lipoic acid-containing food containing the α-lipoic acid powder coating according to claim 2.

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